Method for the production of amorphous rifaximin

a technology of rifaximin and amorphous form, which is applied in the field of amorphous rifaximin production, can solve the problems of change form, unstable several forms, and serious consequences on maintaining the desired properties, and achieves the effects of increasing the solubility of amorphous forms, enhancing drug bioavailability, and increasing the solubility valu

Active Publication Date: 2012-11-15
UNILAB S A S DI LAVAGNA SILVIO MASSIMO & C
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009]In a wholly surprisingly way the inventors have succeeded in obtaining a new amorphous form of stable and pharmaceutically active rifaximin, different from other amorphous forms known up to now, with a maximum solubility measurable in water and a kinetics of solubization in water higher than other amorphous and crystalline forms of rifaximin known to the state of art. The higher solubility of this amorphous form is an advantage for all pharmaceutical applications as a high solubility value enhances the drug bioavailability; the higher solubility kinetics enhances the speed thereof therewith such drug reaches the effective concentrations.

Problems solved by technology

Furthermore, the stability of the several forms can have very serious consequences upon maintaining the wished properties, such as the therapeutic efficiency in case of a molecule used as drug.
When it appears in spontaneous form, the tendency to change form represents a disadvantage for a compound used as pharmaceutical active principle therefor it is a fundamental requirement, the stability in a specific polymorphous form.

Method used

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  • Method for the production of amorphous rifaximin
  • Method for the production of amorphous rifaximin
  • Method for the production of amorphous rifaximin

Examples

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example 1

[0094]0.7 grams of rifaximin are placed in powder into a jar of the free volume of 40 cm3 and added with 2 12-mm-wide steel marbles (unitary mass 7.12 grams). The jar is closed and made integral to an apparatus of “shaker” type, actuated at about 900 revolutions / minute, equal to a frequency of impacts of about 60 impacts per second. Under optimum conditions the obtained energy transfer is in the order of 90-100 mJ per impact. The time length of the mechano-chemical action is equal to 15 minutes. The recovered material has amorphous structure and shows the XRD pattern shown in FIG. 2.

example 2

[0095]0.5 grams of rifaximin are placed in powder into a jar of the free volume of 40 cm3 and added with 4 8-mm-wide marbles of zirconium oxide (ZrO2) (unitary mass 1.63 grams). The jar is closed and made integral to an apparatus of “shaker” type, actuated at about 900 revolutions / minute, equal to an impact frequency of about 120 impacts per second. Under optimum conditions the obtained energy transfer is in the order of 20-25 mJ per impact. The time length of the mechano-chemical action is equal to 60 minutes. The recovered material has amorphous structure and shows the XRD pattern shown in FIG. 3.

example 3

[0096]1 gram of rifaximin is placed in powder into a jar of the free volume of 40 cm3 and added with 4 10-mm-wide marbles of zirconia (ZrO2) (unitary mass 3.06 grams). The jar is closed and made integral to an apparatus of “shaker” type, actuated at about 900 revolutions / minute, equal to an impact frequency of about 120 impacts per second. Under optimum conditions the obtained energy transfer is in the order of 40-50 mJ per impact. The time length of the mechano-chemical action is equal to 60 minutes. The recovered material has amorphous structure and shows the XRD pattern shown in FIG. 4.

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Abstract

The present invention relates to a new amorphous form of rifaximin and to methods for the preparation thereof by means of high energy milling or Spray drying. The present invention further relates to a new amorphous form for use as medicament and to the pharmaceutical compositions composing it.

Description

[0001]The present invention relates to a new amorphous form of rifaximin and to methods for the production thereof by means of high energy milling or Spray drying. The present invention also relates to the new amorphous form for use as a medicament and to the pharmaceutical compositions comprising it.STATE OF PRIOR ART[0002]The phenomenon of polymorphism in chemistry is generated by the possibility that the same molecule organizes in different (polymorphic) crystals, crystallizes with solvent molecules (hydrates and solvates) or solidifies without periodicity (amorphous). The different crystalline or amorphous phases, even if they contain the same active molecule, can have even very different chemical, physical and mechanical properties with huge consequences upon the use thereof as active principles. In particular different solid forms show different chemical activities against other substances, which explicates with particular evidence in case of solvent or dispersing agents. Furt...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07D498/22A61P31/00A61K31/437
CPCC07D498/22A61P31/00A61P31/04
Inventor LAVAGNA, SILVIO MASSIMOSECCI, DANIELAPADELLA, FRANCO
Owner UNILAB S A S DI LAVAGNA SILVIO MASSIMO & C
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